OPTIMIZATION OF RIVASTIGMINE CHITOSAN NANOPARTICLES FOR NEURODEGENERATIVE ALZHEIMER; IN VITRO AND EX VIVO CHARACTERIZATIONS

Objective: In an attempt to optimize the anti-Alzheimer effect, rivastigmine-loaded chitosan nanoparticles were developed in order to target of brain through skin permeation. Methods: Rivastigmine-loaded chitosan-tripolyphosphate nanoparticles were prepared by modified ionic gelation method using tween 80 surfactants in different batches with variable chitosan/cross-linker ratios, desirability factors were applied to choose the optimal Nanocarrier and (F15) was selected. Different rivastigmine concentrations were loaded and the highest encapsulation efficiency formulae chosen for further study and evaluated by scanning electron microscopy (SEM), transmission electron microscopy (TEM) and differential scanning calorimetric (DSC). Further, drug loading, Ex-vivo skin permeation of Nano-gel, and kinetic studies were carried out in addition to stability along three months under different temperature. Results: Particle size and polydispersity index showed average 291.6±7.70 to 490.6±7.42 d. nm. and 0.333±0.04 to 0.570±0.023 respectively. The nanoparticles were spherical in shape. Drug concentrations 4% w/w showed the highest drug entrapment efficiency (89.80%) and drug loading (40.81). Ex vivo studies shows that gel formulae of rivastigmine loaded chitosan nanoparticles was not irritant to rat skin had better skin permeation than chitosan nanoparticles aqueous dispersion also capable of releasing the drug in a sustained manner, and follow kinetic diffusion model. Optimum formula F15 was physical and chemical stable. Conclusion: The experimental results showed the suitability of chitosan nanoparticles coated with a surfactant as a potential carrier for permeation through skin and brain, providing sustained delivery of rivastigmine.

CYCLODEXTRIN INCLUSION COMPLEXES OF PHARMACEUTICALLY ACTIVE DERIVATIVES OF THE CYTISINE ALKALOID AND THEIR HEMORHEOLOGICAL ACTIVITY

The alkaloid cytisine is of great importance for modern pharmacological studies. This alkaloid can be used as a component of the supramolecular system with cyclic oligosaccharides, namely β-cyclodextrins, which have a truncated cone-shaped molecule with internal protons Н3 and Н5 and external ones Н2 and Н4. The aim of the work is to obtain inclusion complexes of pharmaceutically active derivatives of the alkaloid cytisine. The inclusion complexes of cytisine alkaloid derivatives with β-CD and 2-HP-β-CD were obtained by the coprecipitation method. Thermogravimetric, differential thermal, and differential scanning calorimetric analyzes were performed. It was shown that inclusion complexes of substrate with cyclodextrin cavity of receptors were formed. The greatest change in the chemical shifts of protons during the formation of supra-molecular complexes occurs with the internal protons H-3 and H-5 of the cyclodextrin cavity. All calculated values are in good agreement with experimental data. The prepa-ration of supramolecular complexes has been proven using a variety of physicochemical methods of analysis. According to DSC data, the process of complexes destruction in the temperature range of 30-610°C was studied in comparison with the data of the initial cyclodextrin. The hemorheological effects of the investigated samples were studied in vitro. Among four samples studied, two samples showed the ability to reduce blood viscosity in vitro in the blood hyperviscosity model.

Effects of maltodextrin on physicochemical properties of freeze-dried avocado powder

The effect of maltodextrin on the moisture sorption isotherm, glass transition temperature (Tg), and degree of caking of freeze-dried avocado samples at room temperature (25°C) was investigated. The incorporation of maltodextrin reduced the water sorption capacity of the powder due to its less hygroscopic nature. Parameters derived from the Guggenheim, Anderson, and de Boer (GAB) model describing the properties of absorbed water are discussed. The water absorption isotherm possessed the characteristic sigmoid-shaped type II isotherm curves and the model gave the best fit over the whole range of aw tested. The differential scanning calorimetric method was used to measure the Tg of freeze-dried avocado samples. Increasing the water content decreased the Tg, and Tg was increased with increasing maltodextrin content. Increased maltodextrin content to solid material in the freeze-dried sample was associated with less sensitivity to caking as evidenced by Tg values. In addition, increased maltodextrin content in the powders caused brighter, less yellowish, and more greenish coloration and protected color change including browning index. The antioxidant capacity was significantly decreased with increasing maltodextrin content. Thus, the effect of maltodextrin concentration on physicochemical properties was a promising way to preserve the physical property and chemical compounds in freezedried avocado powder.

Synergistic interaction of renewable nipagin and eugenol for aromatic copoly(ether ester) materials with desired performance

Naturally occurring nipagin and eugenol were used as the collaborative starting materials for poly(ether ester) polymers. In this study, two series of nipagin and eugenol-derived copoly(ether ester)s, PHN11−xE1x and PHN11−xE2x (x = 0%, 5%, 10%, 15%, 20%), were prepared with renewable 1,6-hexanediol as a comonomer. The nipagin-derived component acts as the renewable surrogate of petroleum-based dimethyl terephthalate (DMT), while the eugenol-derived component acts as the cooperative property modifier of parent homopoly(ether ester) PHN1. 1,6-Hexanediol was chosen as the spacer because of its renewability, high boiling point, and short chain to enhance the glass transition temperatures (Tgs) of materials. The molecular weights and chemical structures were confirmed by gel permeation chromatograph (GPC), NMR and FTIR spectroscopies. Thermal and crystalline properties were studied by thermal gravimetric analysis (TGA), differential scanning calorimetric (DSC) and wide-angle X-ray diffraction (WXRD). The tensile assays were conducted to evaluate the mechanical properties. The results suggested that properties of this kind of poly(ether ester)s could be finely tuned by the relative content of two components for the desired applications (elastomer, rubbery) suitable for different scenarios from polyethylene glycol terephthalate (PET) and polybutylene terephthalate (PBT).

Efficient Eco-Friendly Nano-Extracted Gelatin as Biodegradable Packaging Material

Extracted gelatin from the waste of fresh and grilled chicken skin was used to prepare films as a biodegradable packaging material from solutions of various gelatin concentrations using a casting approach. The thermal behavior of extracted gelatins was investigated by differential scanning calorimetric. The particle size and zeta potential of dispersed nanoparticles of gelatins were measured by dynamic light scattering. The surface area of lyophilized gelatin nanoparticles was calculated from the adsorption of N2 gas. Mechanical properties, water vapor permeability (WVP), and oil uptake (OU) of all manufactured films were studied. Tensile strength values significantly increased for films manufactured from both gelatin sources when the concentration increased from 4 % to 6 % up to 5.1 MPa. The elongation of waste skin gelatin-based films was higher than waste grilled skin gelatin (WG)-based films using 4 % and 8 % concentrations up to 57 %. Films manufactured from WG had significantly lower WVP than waste skin gelatin (WS) analogous at a 4 % gelatin concentration. The WVP of films manufactured from gelatin significantly increased as gelatin concentration increased where OU showed higher oil resistance for films manufactured from WS up to 91 % using 4 % gelatin concentration. The morphological structure of the gelatin film was investigated with scanning electron microscopy (SEM). A homogenized and smooth film surface was observed. The percentage of heavy metal was examined by inductively coupled plasma (ICP). The results of this study showed that the films manufactured using higher concentrations of gelatin possessed promising mechanical properties, good barrier properties, and high safety as a recommended biopolymer packaging material for food contact and pharmaceutical applications.

Monoolein Cubic Phase Including Hydrophobized Modified Gelatin and Poly(ethyleneimine) and Its Effect on the Stability of Retinyl Palmitate

Retinyl palmitate (RP) was added in monoolein (MO) cubic phase including decanoyl poly(ethyleneimine) (DePEI) and decanoyl gelatin (DeGel) in its water channel. RP, DePEI, and DeGel was incorporated In the cubic phase without structural disintegration, as confirmed by transmission electron microscopy. Differential scanning calorimetric and polarized optical microscopic analysis showed that adding the additives reduces phase transition temperature of cubic phase by 2 °C to 3 °C. The time-dependent chemical stability of RP added in the cubic phase was analyzed for 4 weeks at 5 °C, 20 °C, 30 °C, and 40 °C, using RP loaded in o/w emulsion as a control. The chemical stability of RP added in cubic phase containing DePEI and DeGel was somewhat higher as compared to the RP added in the cubic phase without DeGel/DePEI, possibly because DeGel/DePEI complex might shield RP from its environment by blocking the water channels inside the cubic phase. Moreover, the chemical stability of RP added in the cubic phase was comparatively higher than RP added in o/w emulsion.

Carboxyl graphene reinforced melamine-based polyamide nanocomposites

Over the years, various types of techniques have been used for the synthesis of nanocomposites. In this work, melamine-based polyamide (PA) was synthesized using a one-pot polycondensation method under mild conditions. carboxyl graphene (CG)/PA nanocomposites (CGMPA) were prepared by CG nanofiller loadings of 1, 3, and 5 wt.% via delamination/adsorption approach. The prepared CGMPA nanocomposites were characterized using different analyses, such as Fourier transform infrared techniques (FTIR), field emission scanning electron microscopy (FESEM), X-ray diffraction (XRD), differential scanning calorimetric (DSC), and thermogravimetric analysis (TGA). The effects of the CG on the thermal properties of the CGMPA nanocomposites were significant. The results showed that the melting temperature (Tm) of neat PA and CGMPA were increased from 378°C to 393°C suggested better dispersion of CG in PA matrix. The decomposition temperature of PA was increased from 451°C to 463°C in CGMPA nanocomposites indicates the better thermal stability of PA matrix by addition of CG.

Differential scanning calorimetric investigations of three rotary nickel-titanium instrument systems before and after simulated clinical uses

Background The transformation temperatures were important values, influencing the mechanical properties and clinical performance of nickel-titanium instruments. The aim of this study was to determine the transformation temperatures of three rotary nickel-titanium (NiTi) instruments: Reciproc, HyFlex CM Pro, and Neoniti before and after simulated clinical uses. Methods Ninety new NiTi instruments of three single-file instruments: Reciproc, HyFlex CM Pro, and Neoniti were divided into three groups. Thirty instruments of each group were divided into 3 subgroups (10 instruments for each subgroup): new, one-time simulated clinical used and sterilised, and three times simulated clinical used and sterilized subgroups. The instruments were in the as-received condition for the new subgroups, one time used in the plastic endo-training blocks and sterilised for the one-time subgroups, and three times used in the plastic endo-training blocks and sterilised for the three times subgroups. Each instrument in subgroups was cut into four small segments of 4–5 mm. All segments of instruments were analysed using Differential Scanning Calorimetry (DSC). Data was collected and analysed using SPSS version 20.0 with ANOVA test or Kruskal–Wallis test at the significant level of 0.05. Results There was not significant difference between before and after simulated clinical use with sterilised procedure in three NiTi instrument systems. The austenite-finish (Af) temperatures of three instrument systems were higher than that of the human body (37 °C), of these, the Af temperature of Neoniti was highest and that of HyFlex CM Pro was lowest. Conclusions The austenite-finish (Af) temperatures of three NiTi instruments were higher than that of human body temperature, therefore, material was in the phase transformation from martensite to austenite, gives the instruments more flexibility when used in the clinical situation.

Role of Zingiber Officinale Essential Oil- Chitosan Based Biopolymer Film For Bioactive Packaging

The recent interest in bio-packing at field of food become trending in the development of antimicrobial coatings. The focus of this study was to assess the potential application of zingiber officinale essential oil (GEO) in chitosan films (CHf). The data indicated that there were significant differences(p < 0.05) in the chemical composition of the samples.Forty-seven active compounds of the essential oil were identified from the rhizomes of ginger, which were identified byGC-MS. Fourier transforms infrared spectra (FT-IR) confirmed that an interaction between the hydroxyl groups of the phenolic compounds of the essential oil and the amide groups of polymer matrix. As shown the appearance of peaks at wavenumbers 1639cm-1 and 1558cm-1 Furthermore, X-ray diffraction results suggested a lower crystallintiyin CHf due to GEO effect. Differential Scanning Calorimetric (DSC) analysis revealed that CHf possessed high thermal stability, especially when different concentrations of GEO added. The bioactive CHf showed distinct activity against both positive and negative gram bacteria. They are Staphylococcus aurous, Bacillus subtillis, Streptococcus Sp. Escherichia coli, Salmonella Sp. Pseudomonas erugiosa. This results provides a comprehensive insight on the importance of films incorporated with EOs of interest in food packaging.

Influence of Component Ratio on Thermal and Mechanical Properties of Terpenoid-Sulfur Composites

Terpenoids are potentially sustainable replacements for petrochemical olefins. Sulfur is a waste product produced in large quantities from fossil fuel refining. Several composites with attractive properties have recently been made from terpenoids and sulfur. This report details the extent to which the ratio of sulfur to terpenoid and the terpenoid olefin content influences the thermal and mechanical properties of such terpenoid-sulfur composites. The terpenoids selected were diunsaturated geraniol and triunsaturated farnesol that, upon their inverse vulcanization with elemental sulfur, yield composites GerSx and FarSx, respectively (x = wt % sulfur). The wt % sulfur in the monomer feed was varied from 30–95 for this study, providing twelve materials. Mechanical analysis of these materials was undertaken by compressive and tensile strength techniques. Differential scanning calorimetric analysis revealed both polymeric and orthorhombic sulfur present in the materials with glass transition temperatures (Tg) of −37 °C to −13 °C and melt temperatures (Tm) of 119 to 104 °C. The crystallinity of composites decreases as the weight fraction of sulfur decreases and composites having the highest olefin content exhibit no detectable crystalline microstructures. The compressive strength of the materials showed increasing strength for higher olefin-content materials for both GerSx (with compressive strength of up to 32 MPa) and FarSx (with compressive strength of up to 43 MPa). The improved strength with increasing olefin content levels off at around 80–85% of terpenoid, after which point both tensile and compressive strength diminish.